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Km Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) AMPK (1) Anaplastic lymphoma kinase (ALK) (1) Angiotensin-converting Enzyme (ACE) (1) Apoptosis (5) Cathepsin (1) DGK (2) EGFR (1) Endogenous Metabolite (4) FLT3 (2) Histone Demethylase (4) HIV (1) ICMT (1) Mitochondrial Metabolism (4) Phosphatase (2) PKA (2) PKC (2) Proton Pump (1) STAT (1) Syk (2) Trk Receptor (3) URAT1 (2)
By Research Areas:	Cancer (22) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (6) Metabolic Disease (3)

Inhibitors & Agonists

Fluorescent Dye

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-148685

KM04416	Others	Cancer
KM04416, an isothiazolone derivative, is a potent glycerol-3-phosphate dehydrogenase (GPD2) inhibitor. KM04416 significantly inhibits PNT1A cell proliferation .

HY-W276106

KM02894	Others	Cancer
KM02894 is an inhibitor of glutamate release. Cancer cells release high levels of glutamate, which disrupts normal bone turnover and may lead to cancer-induced bone pain. KM02894 can be used for cancer related research .

HY-P1597

Malantide	PKA PKC	Cancer
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a *K_m* of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a *K_m* of 16 μM .

HY-157116

ICMT-IN-48	ICMT	Cancer
ICMT-IN-48 (compound 1) is an ICMT inhibitor that is competitive (Km=13 μM) for the prenylated methyl acceptor, the first substrate of ICMT. ICMT-IN-48 inhibits ICMT activity with IC₅₀s affected by the concentration of the second substrate S-adenosylmethinine (SAM), and the IC₅₀s are 3.5 μM (1×Km SAM) and 2.3 μM (10×Km SAM), respectively .

HY-144321

Trk-IN-9	Trk Receptor	Cancer
Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers .

HY-15258

Lesinurad 1 Publications Verification RDEA594	URAT1	Metabolic Disease
Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with *K_m* values of 0.85 and 2 µM, respectively.

HY-15258A

Lesinurad sodium 1 Publications Verification RDEA-594 sodium	URAT1	Metabolic Disease
Lesinurad sodium is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with *K_m* values of 0.85 and 2 µM, respectively.

HY-135474

KM91104

1 Publications Verification

Proton Pump Inflammation/Immunology

KM91104, a cell-permeable V-ATPase inhibitor, specifically targets the a3-b2 subunits of V-ATPase .

KM91104 1 Publications Verification	Proton Pump	Inflammation/Immunology
KM91104, a cell-permeable V-ATPase inhibitor, specifically targets the a3-b2 subunits of V-ATPase .

HY-P1597A

Malantide TFA	PKA PKC	Cancer
Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a *K_m* of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a *K_m* of 16 μM .

HY-163004

*Type II TRK inhibitor* 2**	Trk Receptor	Cancer
Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA ^G595R and Ba/F3-TRKA ^G667C cell proliferation (IC₅₀: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .

HY-D1634

Bz-FVR-AMC	Cathepsin	Others
Bz-FVR-AMC is a fluorogenic substrate for procathepsin with a k_cat/K_m value of 1070 mM ^-1s ^-1. The high concentration of BZ-FVR-AMC inhibits the substrate .

HY-N0751

Scutellarin 5+ Cited Publications	STAT Akt HIV	Infection Cancer
Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and *HIV-1KM018* with EC₅₀s of 26 μM, 253 μM and 136 μM, respectively.

HY-128424

4'-Deoxyphlorizin	Others	Metabolic Disease
4'-Deoxyphlorizin is an inhibitor of the glucose transport system. 4'-Deoxyphlorizi has good phlorizin hydrolase inhibitory activity with the *K_m* value of 0.59 nM and the K_i value of 0.33 nM, respectively .

HY-154986

*MARK4 inhibitor* 2**	AMPK	Cancer
MARK4 inhibitor 2 is an inhibitor of microtubule affinity-regulating kinase 4 (MARK4) with an *K_m* of 6.3×10 ⁷ and an IC₅₀ of 0.82 μM. MARK4 inhibitor 2 inhibits the growth of human cells and can be used for cancer research .

HY-137465

CG428	Trk Receptor	Cancer
CG428 is a potent and selective tropomyosin receptor kinase (TRK) degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells (DC₅₀ = 0.36 nM) and inhibits downstream PLCγ1phosphorylation (IC₅₀ = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (K_d = 1 nM, 28 nM and 4.2 nM, respectively). In addition, CG428 effectively inhibits KM12 cell growth (IC₅₀ = 2.9 nM) .

HY-W012159

Methionylserine H-MET-SER-OH	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
Methionylserine (H-MET-SER-OH) is a methionine- and serine-containing dipeptide. Methionylserine binds to and translocation via intestinal di/tri-peptide transporter 1 (hPEPT1) with a *K_m* value of 0.2 mM. Methionylserine inhibits ACE enzyme activity. Methionylserine can be used in the research of hypension .

HY-113039

L-2-Hydroxyglutaric acid (S)-2-Hydroxyglutaric acid	Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite	Cancer
L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with K_m and K_i of 2.52 mM and 11.13 mM, respectively .

HY-N11653

Bipolal Km 01	Others	Others
Bipolal (KM 01) is a natural product isolated from the culture fluid of bipolar algae (Bipolaris sp.). It has a bipolar structure and can form a surfactant between water and oil, so it has excellent Anti-pollution properties. Bipolal can effectively inhibit marine bioaccumulation and biocorrosion, and has broad application prospects .

HY-W015114

L-2-Hydroxyglutaric acid disodium (S)-2-Hydroxyglutaric acid disodium	Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite	Cancer
L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with K_m and K_i of 2.52 mM and 11.13 mM, respectively .

HY-12067

R406 Maximum Cited Publications 22 Publications Verification	Syk FLT3 Apoptosis	Inflammation/Immunology Cancer
R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk kinase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 reduces immune complex-mediated inflammation . R406 also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM) .

HY-131244

ALK-IN-9	Anaplastic lymphoma kinase (ALK)	Cancer
ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC₅₀s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively .

HY-11108

R406 free base Maximum Cited Publications 22 Publications Verification	Syk FLT3 Apoptosis	Inflammation/Immunology Cancer
R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk kinase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 free base reduces immune complex-mediated inflammation . R406 free base also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM) .

HY-143288

NTPDase-IN-2	Phosphatase	Infection Inflammation/Immunology Cancer
NTPDase-IN-2 (compound 5g) is a selective NTPDase inhibitor with IC₅₀s of 0.04 and 2.27 µM for h-NTPDase-2/-8, respectively. NTPDase-IN-2 non-competitively inhibits h-NTPDase-1/-2 with a *K_m* of 74 µM for h-NTPDase-2. NTPDase-IN-2 can be used in studies of cancer, immunologic disorders as well as bacterial infections .

HY-143287

NTPDase-IN-1	Phosphatase	Infection Inflammation/Immunology Cancer
NTPDase-IN-1 (compound 5a) is a selective NTPDase inhibitor with IC₅₀s of 0.05, 0.23 and 0.54 µM for h-NTPDase-1/-2/-8, respectively. NTPDase-IN-1 non-competitively inhibits h-NTPDase-1/-2 with a *K_m* of 21 µM for h-NTPDase-1. NTPDase-IN-1 can be used in studies of cancer, immunologic disorders as well as bacterial infections .

HY-18750

Zorifertinib 5 Publications Verification AZD3759	EGFR Apoptosis	Cancer
Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At K_m ATP concentrations, the IC₅₀s are 0.3, 0.2, and 0.2 nM for EGFR ^wt, EGFR ^L858R, and EGFR ^{exon 19Del}, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .

HY-113039R

L-2-Hydroxyglutaric acid (Standard) (S)-2-Hydroxyglutaric acid (Standard)	Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite	Cancer
L-2-Hydroxyglutaric acid (Standard) is the analytical standard of L-2-Hydroxyglutaric acid. This product is intended for research and analytical applications. L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with K_m and K_i of 2.52 mM and 11.13 mM, respectively .

HY-W015114R

L-2-Hydroxyglutaric acid disodium (Standard) (S)-2-Hydroxyglutaric acid disodium (Standard)	Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite	Cancer
L-2-Hydroxyglutaric acid (disodium) (Standard) is the analytical standard of L-2-Hydroxyglutaric acid (disodium). This product is intended for research and analytical applications. L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with K_m and K_i of 2.52 mM and 11.13 mM, respectively .

HY-121638A

(5Z,2E)-CU-3 1 Publications Verification	Apoptosis DGK	Cancer
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC₅₀ value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a *K_m* value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .

HY-121638

CU-3	Apoptosis DGK	Inflammation/Immunology Cancer
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC₅₀ value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a *K_m* value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .

Bz-FVR-AMC	Chromogenic Substrates
Bz-FVR-AMC is a fluorogenic substrate for procathepsin with a k_cat/K_m value of 1070 mM ^-1s ^-1. The high concentration of BZ-FVR-AMC inhibits the substrate .

Malantide	PKA PKC	Cancer
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a *K_m* of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a *K_m* of 16 μM .

Malantide TFA	PKA PKC	Cancer
Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a *K_m* of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a *K_m* of 16 μM .

Methionylserine H-MET-SER-OH	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
Methionylserine (H-MET-SER-OH) is a methionine- and serine-containing dipeptide. Methionylserine binds to and translocation via intestinal di/tri-peptide transporter 1 (hPEPT1) with a *K_m* value of 0.2 mM. Methionylserine inhibits ACE enzyme activity. Methionylserine can be used in the research of hypension .

Scutellarin 5+ Cited Publications	Infection Structural Classification Flavonoids Scutellaria baicalensis Georgi Classification of Application Fields Flavones Labiatae Source classification Phenols Polyphenols Plants Disease Research Fields	STAT Akt HIV
Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and *HIV-1KM018* with EC₅₀s of 26 μM, 253 μM and 136 μM, respectively.

L-2-Hydroxyglutaric acid disodium (S)-2-Hydroxyglutaric acid disodium	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields Cancer	Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite
L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with K_m and K_i of 2.52 mM and 11.13 mM, respectively .

L-2-Hydroxyglutaric acid (S)-2-Hydroxyglutaric acid	Structural Classification Microorganisms Classification of Application Fields Anti-aging Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields Cancer	Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite
L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with K_m and K_i of 2.52 mM and 11.13 mM, respectively .

L-2-Hydroxyglutaric acid (Standard) (S)-2-Hydroxyglutaric acid (Standard)	Structural Classification Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite	Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite
L-2-Hydroxyglutaric acid (Standard) is the analytical standard of L-2-Hydroxyglutaric acid. This product is intended for research and analytical applications. L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with K_m and K_i of 2.52 mM and 11.13 mM, respectively .

L-2-Hydroxyglutaric acid disodium (Standard) (S)-2-Hydroxyglutaric acid disodium (Standard)	Structural Classification Ketones, Aldehydes, Acids Source classification Endogenous metabolite	Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite
L-2-Hydroxyglutaric acid (disodium) (Standard) is the analytical standard of L-2-Hydroxyglutaric acid (disodium). This product is intended for research and analytical applications. L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with K_m and K_i of 2.52 mM and 11.13 mM, respectively .

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Km Inhibitors

Inhibitors & Agonists

Fluorescent Dye

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